II. Indications
- Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
- Typically used in combination with 5-HT3 Antagonists and Dexamethasone 20 mg daily
III. Mechanism
- Blocks the neurokinin-1 receptor (a tachykinin)
- Cross the blood brain barrier to inhibit CNS substance-P activity
- Effects
- Antiemetic (synergistic with 5-HT3 Antagonists)
- Anxiolysis and Antidepressant properties
IV. Dosing
- Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
- Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
- Take 180 mg orally 1 to 2 hours prior to Chemotherapy
-
Postoperative Nausea and Vomiting Prevention (off-label)
- Give 90 to 180 mg orally at Anesthesia induction
VI. Safety
- Unknown safety in pregnancy
- Unknown safety in Lactation
VII. Drug Interactions
- May effect drugs metabolized by CYP2D6
-
Thioridazine
- Avoid with NK1 Receptor Antagonist
- Strong CYP3A4 Inducers (e.g. Rifampin)
- May decrease Rolapitant effectiveness
VIII. Resources
- NK1 Receptor Antagonist (Wikipedia)
- Antiemetic Neurokinin-1 Receptor Blockers (Stat Pearls)
- Rolapitant (DailyMed)
IX. References
- (2023) Postoperative Nausea and Vomiting Management, Presc Lett, #390431
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
- (2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]